Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 99-06-9, Name is 3-Hydroxybenzoic acid, SMILES is O=C(O)C1=CC=CC(O)=C1, belongs to Benzisoxazole compound. In a document, author is Younkin, Jason, introduce the new discover, Application In Synthesis of 3-Hydroxybenzoic acid.
Reformulating a Pharmacophore for 5-HT2A Serotonin Receptor Antagonists
Several pharmacophore models have been proposed for 5-HT2A serotonin receptor antagonists. These typically consist of two aromatic/hydrophobic moieties separated by a given distance from each other, and from a basic amine. Although specified distances might vary, the models are relatively similar in their general construction. Because our preliminary data indicated that two aromatic (hydrophobic) moieties might not be required for such action, we deconstructed the serotonin-dopamine antipsychotic agent risperidone (1) into four smaller structural fragments that were thoroughly examined in 5-HT2A receptor binding and functional (i.e., two-electrode voltage clamp (TEVC) and intracellular calcium release) assays. It was apparent that truncated risperidone analogues behaved as antagonists. In particular, 6-fluoro-3-(1-methylpiperidin-4-yl)benzisoxazole (4) displayed high affinity for 5-HT2A, receptors (K-i, of ca. 12 nM) relative to risperidone (K-i of ca. 5 nM) and behaved as a potent 5-HT2A serotonin receptor antagonist. These results suggest that multiple aromatic (hydrophobic) moieties are not essential for high-affinity 5-HT2A receptor binding and antagonist activity and that current pharmacophore models for such agents are very much in need of revision.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 99-06-9 is helpful to your research. Application In Synthesis of 3-Hydroxybenzoic acid.
Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics